P2Y1 Receptor
P2Y1 receptor is an ADP-responsive platelet GPCR that mediates intracellular Ca2+ mobilization and platelet shape change[1]. Mechanistically, ADP-induced platelet aggregation requires concomitant signaling through P2Y1 and the distinct ADP receptor P2Y12, showing that these isoforms control different components of platelet activation[2]. In mouse models, loss of P2Y1 reduces platelet aggregation, prolongs bleeding time, and increases resistance to thromboembolism[3][4]. Compared with P2Y12, which supports Gi-linked signaling, P2Y1 provides the Gq-linked Ca2+ and shape-change arm required to initiate ADP responses[1][2]. For experimental applications, MRS2500 inhibits platelet aggregation and thrombosis as a potent, selective, stable P2Y1 antagonist[5]. However, nucleotide P2Y1 agonists and antagonists can undergo rapid hydrolysis in plasma and blood, so pharmacological studies should control for active nucleoside metabolites[6].
References:
- [1]. Jin J, et al. Molecular basis for ADP-induced platelet activation. II. The P2Y1 receptor mediates ADP-induced intracellular calcium mobilization and shape change in platelets. J Biol Chem. 1998 Jan 23;273(4):2030-4. [Content Brief]
- [2]. Jin J, et al. Coactivation of two different G protein-coupled receptors is essential for ADP-induced platelet aggregation. Proc Natl Acad Sci U S A. 1998 Jul 7;95(14):8070-4. [Content Brief]
- [3]. Greenspan NS, et al. Defining epitopes: It's not as easy as it seems. Nat Biotechnol. 1999 Oct;17(10):936-7. [Content Brief]
- [4]. Léon C, et al. Defective platelet aggregation and increased resistance to thrombosis in purinergic P2Y(1) receptor-null mice. J Clin Invest. 1999 Dec;104(12):1731-7. [Content Brief]
- [5]. Hechler B, et al. MRS2500 [2-iodo-N6-methyl-(N)-methanocarba-2'-deoxyadenosine-3',5'-bisphosphate], a potent, selective, and stable antagonist of the platelet P2Y1 receptor with strong antithrombotic activity in mice. J Pharmacol Exp Ther. 2006 Feb;316(2):556-63. [Content Brief]
- [6]. Liston TE, et al. Nucleotide P2Y1 receptor agonists are in vitro and in vivo prodrugs of A1/A3 adenosine receptor agonists: implications for roles of P2Y1 and A1/A3 receptors in physiology and pathology. Purinergic Signal. 2020 Dec;16(4):543-559. [Content Brief]
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P2Y1 Receptor Related Products (24)
Related Products (24)
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BPTU
0 ImagesSynonyms: BMS-646786BPTU (BMS-646786) is a non-nucleotide P2Y1 receptor allosteric antagonist with antithrombotic activity. BPTU is able to block the P2Y1 receptor located at the neuromuscular junction of the gastrointestinal tract.
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PIT
0 ImagesSynonyms: 2,2'-Pyridylisatogen tosylatePIT (2,2'-Pyridylisatogen tosylate) is a selective and non-competitive antagonist of P2Y1 receptor with an IC50 value of 0.14 μM for human P2Y1 receptor. PIT antagonizes P2Y1 receptor signaling without affecting nucleotide binding. PIT is an irreversible antagonist of responses to ATP at metabotropic purinoceptors (of the P2Y family) in some smooth muscles. PIT can be used for the research of chronic bronchitis and asthma.
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P2Y14R antagonist 1
0 ImagesP2Y14R antagonist 1 (compound I-17) is a selective P2Y14R antagonist with an IC50 of 0.6 nM. It exhibits potent P2Y14R antagonistic activity, both in vitro and in vivo efficacy, and favorable pharmacokinetic profiles. P2Y14R antagonist 1 reduces the release of inflammatory factors and cell pyroptosis through the NOD-like receptor family pyrin domain-containing 3 (NLRP3)/gasdermin D (GSDMD) signaling pathway. P2Y14R antagonist 1 holds promise for research in the field of acute gouty arthritis.
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MRS2365 trisodium
0 ImagesCat. No.: HY-108656APurity: 99.8%MRS2365 trisodium is a potent and selective P2Y1 receptor (EC50=0.4 nM)/[35S]GTPγS binding/β-arrestin 2 recruitment agonist. MRS2365 trisodium relieves mechanical allodynia and increases mechanical sensitivity.
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Desmodilactone
0 ImagesCat. No.: HY-N18260CAS No.: 60010-74-4Desmodilactone is a P2Y1R allosteric antagonist. Desmodilactone can be used for the research of thrombosis.
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MRS2279 diammonium
0 ImagesCat. No.: HY-108657ACAS No.: 2387505-47-5MRS2279 diammonium is a selective and high affinity P2Y1 receptor antagonist, with a Ki value of 2.5 nM and an IC50 value of 51.6 nM. MRS2279 diammonium competitively inhibits ADP-promoted platelet aggregation with an pKb value of 8.05.
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MRS2365
0 ImagesCat. No.: HY-108656CAS No.: 436847-09-5MRS2365 is a potent and selective P2Y1 receptor (EC50=0.4 nM) /[35S]GTPγS binding/β-arrestin 2 recruitment agonist with an EC50 of 0.4 nM. MRS2365 relieves mechanical allodynia and increases mechanical sensitivity. MRS2365 shows little agonist or antagonist activity at the P2Y12 or P2Y13 receptors.
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MRS2179 tetrasodium
0 ImagesCat. No.: HY-101308CAS No.: 1454889-37-2MRS2179 tetrasodium is a competitive P2Y1 receptor antagonist, with a Kb of 102 nM and a pA2 of 6.99 for turkey P2Y1 receptor. MRS2179 tetrasodium is selective for P2Y1 over P2X1 (IC50=1.15 µM), P2X3 (12.9 µM), P2X2, P2X4, P2Y2, P2Y4, and P2Y6 receptors. MRS2179 tetrasodium inhibits platelet aggregation.
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Adenosine 2',5'-diphosphate sodium
0 ImagesAdenosine 2',5'-diphosphate sodium is a competitive P2Y1 antagonist. Adenosine 2',5'-diphosphate sodium exhibits non-selective antagonism at recombinant and human platelet P2X1 receptors.
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Blue FPG-A trisodium
0 ImagesCat. No.: HY-D1199CAS No.: 78617-94-4Blue FPG-A trisodium is a selective antagonist of P2X1 receptor and P2Y1 receptor with IC50 values of 35.5 μM and 2.6 μM, respectively. Blue FPG-A trisodium is a structural isomer of the components of Reactive Blue 2 (RB2).
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BMS-884775
0 ImagesCat. No.: HY-120612CAS No.: 1557206-59-3BMS-884775 is a selective and orally active P2Y1 antagonist with an IC50 of 0.1 nM for the human P2Y1 receptor. BMS-884775 has a similar efficacy in preventing arterial thrombosis to Clopidogrel (HY-15283) and Prasugrel (HY-15284), but treatment with BMS-884775 results in shorter bleeding time and lower bleeding risk. BMS-884775 can be used in research related to antiplatelet and arterial thrombosis-associated diseases.
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MRS-2179
0 ImagesCat. No.: HY-115273CAS No.: 101204-49-3MRS-2179 is a selective and competitive antagonist for P2Y1 receptor, with KB of 0.177 μM.
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TNP-ATP tetrasodium
0 ImagesCat. No.: HY-137610ATNP-ATP is an antagonist of purinergic P2Y1, P2X3, and P2X2/3 receptors (IC50 = 6, 0.9, and 7 nM, respectively, in HEK293 cells expressing human receptors). TNP-ATP reduces acetate-induced calcium flux in 1321N1 cells expressing P2X3 and P2X2/3 receptors (IC50 = 100 and 62 nM, respectively). TNP-ATP dose-dependently attenuates acetate-induced abdominal contractions in a mouse visceral pain model (ED50 = 6.35 µmol/kg)[1][2].
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P2Y1 antagonist 4
0 ImagesCat. No.: HY-175675CAS No.: 3104888-50-5P2Y1 antagonist 4 is a selective P2Y1 receptor antagonist with excellent blood-brain barrier (BBB) penetration. P2Y1 antagonist 4 inhibits P2Y1 receptor-mediated cytosolic Ca2+ increase (IC50 = 1.95 μM) and platelet aggregation (IC50 = 3.24 μM) induced by ADP in rabbit washed platelets. P2Y1 antagonist 4 significantly upregulates the level of nuclear Nrf2 protein in H2O2-treated HT22 cells. P2Y1 antagonist 4 reduces myocardial infarct size in a mouse acute myocardial infarction (MI) model. P2Y1 antagonist 4 can be used for the study of ischemic stroke and myocardial infarction.
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P2Y1/P2Y6 antagonist 1
0 ImagesCat. No.: HY-176143P2Y1/P2Y6 antagonist 1 (Compound 3h) is an indolesulfonylhydrazide derivative. P2Y1/P2Y6 antagonist 1 is an orally active tP2Y1 and rP2Y6 antagonist (IC50 of 9.72 and 1.89 μM, respectively). P2Y1/P2Y6 antagonist 1 can be used in the study of neurological diseases, inflammation, cardiovascular diseases and cancer.
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Adenosine 3'-phosphate 5'-phosphosulfate lithium, hydrate
0 ImagesCat. No.: HY-W250153AAdenosine 3'-phosphate 5'-phosphosulfate lithium hydrate, an adenine nucleotide derivative, is a selective P2Y1 antagonist with no effect on P2Y2, P2Y4, or P2Y6 receptors. Adenosine 3'-phosphate 5'-phosphosulfate lithium hydrate can competitive inhibit ADP-induced platelet aggregation, as well as the ability of ADP to cause shape change and increases in Ca2+ in platelets, but had no effect on the inhibition of stimulated adenylate cyclase by ADP. Adenosine 3'-phosphate 5'-phosphosulfate lithium hydrate is a co-substrate used for the sulfonation of glycans. Adenosine 3'-phosphate 5'-phosphosulfate lithium hydrate can be used for Golgi-resident PAP-specific 3'-phosphatase-coupled sulfotransferase assays, which as donor substrate to transfer a sulfonate group.
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MRS2279
0 ImagesCat. No.: HY-108657CAS No.: 367909-40-8MRS2279 is a selective and high affinity P2Y1 receptor antagonist, with a Ki of 2.5 nM and an IC50 of 51.6 nM. MRS2279 competitively inhibits ADP-promoted platelet aggregation with an apparent affnity (pKB=8.05).
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P2Y1 antagonist 1
0 ImagesCat. No.: HY-120636CAS No.: 1555697-67-0P2Y1 antagonist 1 (compound 10q) is a potent antagonist of P2Y1, with the IC50s of 1.1 nM and 0.24 μM in FLIPR assay and hPA assay, respectively. P2Y1 antagonist 1 plays an important role in antiplatelet research.
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Adenosine 3'-phosphate 5'-phosphosulfate
0 ImagesAdenosine 3'-phosphate 5'-phosphosulfate, an adenine nucleotide derivative, is a selective P2Y1 antagonist with no effect on P2Y2, P2Y4, or P2Y6 receptors. Adenosine 3'-phosphate 5'-phosphosulfate can competitive inhibit ADP-induced platelet aggregation, as well as the ability of ADP to cause shape change and increases in Ca2+ in platelets, but had no effect on the inhibition of stimulated adenylate cyclase by ADP. Adenosine 3'-phosphate 5'-phosphosulfate is a co-substrate used for the sulfonation of glycans. Adenosine 3'-phosphate 5'-phosphosulfate can be used for Golgi-resident PAP-specific 3'-phosphatase-coupled sulfotransferase assays, which as donor substrate to transfer a sulfonate group.
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